Imidazo-pyrazine derivatives as potent CXCR3 antagonists

A general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. Optimization efforts led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetic properties in addition to increased potency. The efficacy of the lead compound 21 is evaluated in a mouse lung inflammation model.

Graphical abstractA general way of improving the potency of CXCR3 antagonists with fused hetero-bicyclic cores was identified. This led to the discovery of a series of imidazo-pyrazine derivatives with improved pharmacokinetics. Compound 21 was evaluated in a lung inflammation model.Figure optionsDownload full-size imageDownload as PowerPoint slide